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Synthesis, Pim kinase inhibitory potencies and in vitro antiproliferative activities of diversely substituted pyrrolo[2,3-a]carbazoles by Rufine Akué-Gédu; Lionel Nauton; Vincent Théry; Jenny Bain; Philip Cohen; Fabrice Anizon; Pascale Moreau is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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The synthesis of new pyrrolo[2,3-a]carbazole derivatives diversely substituted at the C-6 to C-9 positions is described. These compounds were tested for their kinase inhibitory potencies toward three kinases (Pim-1, Pim-2, Pim-3) as well as for their in vitro antiproliferative activities toward a human fibroblast primary culture and three human solid cancer cell lines (PC3, DU145, and PA 1). Moreover, molecular docking studies were performed to explain the enhanced inhibitory activity of the most active compound 3d.

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Author

Rufine Akué-Gédu; Lionel Nauton; Vincent Théry; Jenny Bain; Philip Cohen; Fabrice Anizon; Pascale Moreau

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2010

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)